A fluopol-ABPP HTS assay to identify PAD inhibitors

作者：Knuckley Bryan; Jones Justin E; Bachovchin Daniel A; Slack Jessica; Causey Corey P; Brown Steven J; Rosen Hugh; Cravatt Benjamin F; Thompson Paul R^*

来源：Chemical communications, 2010, 46(38): 7175-7177.

DOI：10.1039/c0cc02634d

Protein Arginine Deiminase (PAD) activity is dysregulated in numerous diseases, e. g., Rheumatoid Arthritis. Herein we describe the development of a fluorescence polarization-Activity Based Protein Profiling (fluopol-ABPP) based high throughput screening assay that can be used to identify PAD-selective inhibitors. Using this assay, streptonigrin was identified as a potent, selective, and irreversible PAD4 inactivator.

• 出版日期2010